8. Trimeric G Protein Signaling Flashcards
what are the 2 things required to stimulated adenylyl cyclase?
hormone (ligand) & GTP
2 major signaling mechanisms that a cell can use?
- direct phosphorylation
2. signaling via nucleotide-triphosphate-binding to a G protein
GTPase enzyme kinetics
has a low Km (high affinity)
3 subunits of G proteins?
alpha
beta
gamma
G-as
defines the majority of G protein function
activates AC
G-aq
activates PLC-beta
What is the rate limiting step for a reaction with a G protein?
dissociation of GDP from the alpha subunit
G protein, by default, is in what form?
OFF (T-form)
second step proceeds 10x faster when a ligand is not bound to the GPCR
example of G protein signaling: epinephrine
E binds receptor
GDP dissociates, replaced by GTP, activates Gas
Gas activates AC
AC catalyzes formation of cAMP
cAMP activates PKA
PKA phosphorylates cellular proteins that cause the cellular response to E
GPCR structure
7 transmembrane domains
which cytoplasmic loop interacts with the G protein the most?
3rd
receptor is buried within the membrane
what does AC do?
catalyze the formation of cAMP
What does PLC do?
break PIP2 into IP3 & DAG
What activates PLPC-beta
G-alpha-q
Secondary messengers examples (4)
cAMP
IP3
DAG
Calcium